CA3058272A1 - Pharmaceutical composition containing mor agonist and kor agonist, and uses thereof - Google Patents
Pharmaceutical composition containing mor agonist and kor agonist, and uses thereof Download PDFInfo
- Publication number
- CA3058272A1 CA3058272A1 CA3058272A CA3058272A CA3058272A1 CA 3058272 A1 CA3058272 A1 CA 3058272A1 CA 3058272 A CA3058272 A CA 3058272A CA 3058272 A CA3058272 A CA 3058272A CA 3058272 A1 CA3058272 A1 CA 3058272A1
- Authority
- CA
- Canada
- Prior art keywords
- pain
- group
- heterocyclyl
- cycloalkyl
- alkyl
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Abandoned
Links
- 239000000556 agonist Substances 0.000 title claims abstract description 110
- 239000008194 pharmaceutical composition Substances 0.000 title claims abstract description 10
- 208000002193 Pain Diseases 0.000 claims abstract description 173
- 230000036407 pain Effects 0.000 claims abstract description 162
- 108020001612 μ-opioid receptors Proteins 0.000 claims abstract description 61
- 150000001875 compounds Chemical class 0.000 claims abstract description 45
- 150000003839 salts Chemical class 0.000 claims abstract description 23
- 239000000203 mixture Substances 0.000 claims abstract description 21
- 239000003814 drug Substances 0.000 claims abstract description 18
- 108090000137 Opioid Receptors Proteins 0.000 claims abstract description 12
- 102000003840 Opioid Receptors Human genes 0.000 claims abstract description 12
- 238000002360 preparation method Methods 0.000 claims abstract description 10
- 102000051367 mu Opioid Receptors Human genes 0.000 claims abstract 2
- 125000000623 heterocyclic group Chemical group 0.000 claims description 124
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 111
- 125000000217 alkyl group Chemical group 0.000 claims description 96
- -1 nitro, hydroxy Chemical group 0.000 claims description 94
- 125000003118 aryl group Chemical group 0.000 claims description 80
- 125000001072 heteroaryl group Chemical group 0.000 claims description 79
- 125000003545 alkoxy group Chemical group 0.000 claims description 61
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims description 48
- 229910052736 halogen Inorganic materials 0.000 claims description 40
- 150000002367 halogens Chemical class 0.000 claims description 40
- 125000001424 substituent group Chemical group 0.000 claims description 40
- 125000002768 hydroxyalkyl group Chemical group 0.000 claims description 39
- 125000001188 haloalkyl group Chemical group 0.000 claims description 35
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims description 31
- 125000004093 cyano group Chemical group *C#N 0.000 claims description 29
- 229910052739 hydrogen Inorganic materials 0.000 claims description 27
- 239000001257 hydrogen Substances 0.000 claims description 26
- 125000004453 alkoxycarbonyl group Chemical group 0.000 claims description 21
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims description 16
- 208000004296 neuralgia Diseases 0.000 claims description 16
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims description 15
- 229910052757 nitrogen Inorganic materials 0.000 claims description 15
- 206010065390 Inflammatory pain Diseases 0.000 claims description 14
- 125000004438 haloalkoxy group Chemical group 0.000 claims description 14
- 230000000302 ischemic effect Effects 0.000 claims description 13
- 230000000472 traumatic effect Effects 0.000 claims description 13
- 125000005842 heteroatom Chemical group 0.000 claims description 12
- 210000000056 organ Anatomy 0.000 claims description 12
- 238000001356 surgical procedure Methods 0.000 claims description 12
- 206010028980 Neoplasm Diseases 0.000 claims description 10
- 125000003342 alkenyl group Chemical group 0.000 claims description 10
- XGZZHZMWIXFATA-UEZBDDGYSA-N nalfurafine Chemical compound C([C@]12[C@H]3OC=4C(O)=CC=C(C2=4)C[C@@H]2[C@]1(O)CC[C@H]3N(C)C(=O)\C=C\C1=COC=C1)CN2CC1CC1 XGZZHZMWIXFATA-UEZBDDGYSA-N 0.000 claims description 10
- 229960000441 nalfurafine Drugs 0.000 claims description 10
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- 125000004043 oxo group Chemical group O=* 0.000 claims description 5
- 229910052760 oxygen Inorganic materials 0.000 claims description 5
- 230000002062 proliferating effect Effects 0.000 claims description 5
- 125000006239 protecting group Chemical group 0.000 claims description 5
- DYKJMRFQHDXDHH-UHFFFAOYSA-N 2-(3,4-dichlorophenyl)-1-[2-[(3-hydroxypyrrolidin-1-yl)methyl]-4,4-dimethylpiperidin-1-yl]ethanone Chemical compound C1C(C)(C)CCN(C(=O)CC=2C=C(Cl)C(Cl)=CC=2)C1CN1CCC(O)C1 DYKJMRFQHDXDHH-UHFFFAOYSA-N 0.000 claims description 4
- FWMNVWWHGCHHJJ-SKKKGAJSSA-N 4-amino-1-[(2r)-6-amino-2-[[(2r)-2-[[(2r)-2-[[(2r)-2-amino-3-phenylpropanoyl]amino]-3-phenylpropanoyl]amino]-4-methylpentanoyl]amino]hexanoyl]piperidine-4-carboxylic acid Chemical compound C([C@H](C(=O)N[C@H](CC(C)C)C(=O)N[C@H](CCCCN)C(=O)N1CCC(N)(CC1)C(O)=O)NC(=O)[C@H](N)CC=1C=CC=CC=1)C1=CC=CC=C1 FWMNVWWHGCHHJJ-SKKKGAJSSA-N 0.000 claims description 4
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- JAQUASYNZVUNQP-USXIJHARSA-N Levorphanol Chemical compound C1C2=CC=C(O)C=C2[C@]23CCN(C)[C@H]1[C@@H]2CCCC3 JAQUASYNZVUNQP-USXIJHARSA-N 0.000 claims description 4
- 208000005298 acute pain Diseases 0.000 claims description 4
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- 230000001430 anti-depressive effect Effects 0.000 claims description 4
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- JHLHNYVMZCADTC-LOSJGSFVSA-N asimadoline Chemical compound C([C@@H](N(C)C(=O)C(C=1C=CC=CC=1)C=1C=CC=CC=1)C=1C=CC=CC=1)N1CC[C@H](O)C1 JHLHNYVMZCADTC-LOSJGSFVSA-N 0.000 claims description 4
- 229950002202 asimadoline Drugs 0.000 claims description 4
- ZPUCINDJVBIVPJ-LJISPDSOSA-N cocaine Chemical compound O([C@H]1C[C@@H]2CC[C@@H](N2C)[C@H]1C(=O)OC)C(=O)C1=CC=CC=C1 ZPUCINDJVBIVPJ-LJISPDSOSA-N 0.000 claims description 4
- 229950003869 difelikefalin Drugs 0.000 claims description 4
- 210000003414 extremity Anatomy 0.000 claims description 4
- 229960003406 levorphanol Drugs 0.000 claims description 4
- 239000000041 non-steroidal anti-inflammatory agent Substances 0.000 claims description 4
- ABTNETSDXZBJTE-WLHGVMLRSA-N (e)-but-2-enedioic acid;methyl 4-[2-(3,4-dichlorophenyl)acetyl]-3-(pyrrolidin-1-ylmethyl)piperazine-1-carboxylate Chemical compound OC(=O)\C=C\C(O)=O.C1N(C(=O)OC)CCN(C(=O)CC=2C=C(Cl)C(Cl)=CC=2)C1CN1CCCC1 ABTNETSDXZBJTE-WLHGVMLRSA-N 0.000 claims description 3
- 208000004998 Abdominal Pain Diseases 0.000 claims description 3
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- 239000001961 anticonvulsive agent Substances 0.000 claims description 3
- 230000002757 inflammatory effect Effects 0.000 claims description 3
- 239000003589 local anesthetic agent Substances 0.000 claims description 3
- 230000036244 malformation Effects 0.000 claims description 3
- NETZHAKZCGBWSS-CEDHKZHLSA-N nalbuphine Chemical compound C([C@]12[C@H]3OC=4C(O)=CC=C(C2=4)C[C@@H]2[C@]1(O)CC[C@@H]3O)CN2CC1CCC1 NETZHAKZCGBWSS-CEDHKZHLSA-N 0.000 claims description 3
- 229960000805 nalbuphine Drugs 0.000 claims description 3
- 125000004433 nitrogen atom Chemical group N* 0.000 claims description 3
- 229940021182 non-steroidal anti-inflammatory drug Drugs 0.000 claims description 3
- 239000000014 opioid analgesic Substances 0.000 claims description 3
- 239000000546 pharmaceutical excipient Substances 0.000 claims description 3
- 210000001364 upper extremity Anatomy 0.000 claims description 3
- DBOGGOVKHSCMNB-OMRVPHBLSA-N (2r)-2-[[(2r)-2-[[(2r)-2-amino-3-phenylpropanoyl]amino]-3-phenylpropanoyl]amino]-n-[(2r)-5-(diaminomethylideneamino)-1-oxo-1-(pyridin-4-ylmethylamino)pentan-2-yl]hexanamide Chemical compound C([C@H](C(=O)N[C@H](CCCC)C(=O)N[C@H](CCCNC(N)=N)C(=O)NCC=1C=CN=CC=1)NC(=O)[C@H](N)CC=1C=CC=CC=1)C1=CC=CC=C1 DBOGGOVKHSCMNB-OMRVPHBLSA-N 0.000 claims description 2
- RUOXNQGHBFJAES-ZGFBMJKBSA-N (2r)-n-[(2r)-1-amino-5-(diaminomethylideneamino)-1-oxopentan-2-yl]-2-[[(2r)-2-[[(2r)-2-amino-3-phenylpropanoyl]amino]-3-phenylpropanoyl]amino]hexanamide Chemical compound C([C@H](C(=O)N[C@H](CCCC)C(=O)N[C@H](CCCN=C(N)N)C(N)=O)NC(=O)[C@H](N)CC=1C=CC=CC=1)C1=CC=CC=C1 RUOXNQGHBFJAES-ZGFBMJKBSA-N 0.000 claims description 2
- RFTWMVGLYKJUCZ-KRWDZBQOSA-N 1-[(2s)-2-(pyrrolidin-1-ylmethyl)piperidin-1-yl]-2-[4-(trifluoromethyl)phenyl]ethanone Chemical compound C1=CC(C(F)(F)F)=CC=C1CC(=O)N1[C@H](CN2CCCC2)CCCC1 RFTWMVGLYKJUCZ-KRWDZBQOSA-N 0.000 claims description 2
- ZFWNCCCNZIYJAQ-UHFFFAOYSA-N 1-[4-acetyl-2-[(3-hydroxypyrrolidin-1-yl)methyl]piperazin-1-yl]-2-(3,4-dichlorophenyl)ethanone Chemical compound C1N(C(=O)C)CCN(C(=O)CC=2C=C(Cl)C(Cl)=CC=2)C1CN1CCC(O)C1 ZFWNCCCNZIYJAQ-UHFFFAOYSA-N 0.000 claims description 2
- JMBYBVLCYODBJQ-HFMPRLQTSA-N 2-(1-benzofuran-4-yl)-n-methyl-n-[(5r,7s,8s)-7-pyrrolidin-1-yl-1-oxaspiro[4.5]decan-8-yl]acetamide Chemical compound C([C@@H]([C@H](C1)N2CCCC2)N(C)C(=O)CC=2C=3C=COC=3C=CC=2)C[C@]21CCCO2 JMBYBVLCYODBJQ-HFMPRLQTSA-N 0.000 claims description 2
- MVVCJIVSQDJOOR-VKLKMBQZSA-N 2-(2-aminophenyl)-n-[(1s)-2-[(3s)-3-hydroxypyrrolidin-1-yl]-1-phenylethyl]-n-methylacetamide;hydrochloride Chemical compound Cl.C([C@@H](N(C)C(=O)CC=1C(=CC=CC=1)N)C=1C=CC=CC=1)N1CC[C@H](O)C1 MVVCJIVSQDJOOR-VKLKMBQZSA-N 0.000 claims description 2
- LWUQHEXXEFUHHQ-UHFFFAOYSA-N 2-(3,4-dichlorophenyl)-1-[7-(pyrrolidin-1-ylmethyl)-1,4-dioxa-8-azaspiro[4.5]decan-8-yl]ethanone Chemical compound C1=C(Cl)C(Cl)=CC=C1CC(=O)N1C(CN2CCCC2)CC2(OCCO2)CC1 LWUQHEXXEFUHHQ-UHFFFAOYSA-N 0.000 claims description 2
- AEJOEPSMZCEYJN-HXUWFJFHSA-N 2-(3,4-dichlorophenyl)-N-methyl-N-[(1S)-1-phenyl-2-(1-pyrrolidinyl)ethyl]acetamide Chemical compound C([C@@H](N(C)C(=O)CC=1C=C(Cl)C(Cl)=CC=1)C=1C=CC=CC=1)N1CCCC1 AEJOEPSMZCEYJN-HXUWFJFHSA-N 0.000 claims description 2
- OFNGPKCQCHBFRA-TUYUPMGOSA-N 2-(3,4-dichlorophenyl)-n-[(1s,2s)-5-methoxy-2-pyrrolidin-1-yl-1,2,3,4-tetrahydronaphthalen-1-yl]-n-methylacetamide;methanesulfonic acid Chemical compound CS(O)(=O)=O.N1([C@@H]2[C@H](C=3C=CC=C(C=3CC2)OC)N(C)C(=O)CC=2C=C(Cl)C(Cl)=CC=2)CCCC1 OFNGPKCQCHBFRA-TUYUPMGOSA-N 0.000 claims description 2
- SMJRVISIMGPMFJ-VYJAJWGXSA-N 2-[(1S,3S,4S,7S,9R)-9-(2-hydroxyphenyl)-3,9-dimethyl-2,5,8-trioxa-10-azatricyclo[5.2.1.04,10]decan-3-yl]phenol Chemical compound C1([C@]2(C)O[C@@H]3N4[C@H]2OC[C@@H]4O[C@]3(C)C=2C(=CC=CC=2)O)=CC=CC=C1O SMJRVISIMGPMFJ-VYJAJWGXSA-N 0.000 claims description 2
- JKYJSFISYHSNOE-UHFFFAOYSA-N 2-[3-[1-[[2-(3,4-dichlorophenyl)-1-oxoethyl]-methylamino]-2-(1-pyrrolidinyl)ethyl]phenoxy]acetic acid Chemical compound C=1C=C(Cl)C(Cl)=CC=1CC(=O)N(C)C(C=1C=C(OCC(O)=O)C=CC=1)CN1CCCC1 JKYJSFISYHSNOE-UHFFFAOYSA-N 0.000 claims description 2
- LORDFXWUHHSAQU-UHFFFAOYSA-N 3,4,5-trimethoxybenzoic acid [2-(dimethylamino)-2-phenylbutyl] ester Chemical compound C=1C=CC=CC=1C(CC)(N(C)C)COC(=O)C1=CC(OC)=C(OC)C(OC)=C1 LORDFXWUHHSAQU-UHFFFAOYSA-N 0.000 claims description 2
- ACKBGPXURGPUEW-UHFFFAOYSA-N 3-carbamothioylbenzenesulfonic acid [2-(dimethylamino)-2-phenylbutyl] 3,4,5-trimethoxybenzoate Chemical compound NC(=S)C1=CC=CC(S(O)(=O)=O)=C1.C=1C=CC=CC=1C(CC)(N(C)C)COC(=O)C1=CC(OC)=C(OC)C(OC)=C1 ACKBGPXURGPUEW-UHFFFAOYSA-N 0.000 claims description 2
- FHFHNAQEPILWDK-FCHUYYIVSA-N 4-[[(1s)-2-[(3s)-3-hydroxypyrrolidin-1-yl]-1-phenylethyl]-methylamino]-n-propylbenzamide Chemical compound C1=CC(C(=O)NCCC)=CC=C1N(C)[C@@H](C=1C=CC=CC=1)CN1C[C@@H](O)CC1 FHFHNAQEPILWDK-FCHUYYIVSA-N 0.000 claims description 2
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- VQLPLYSROCPWFF-QZTJIDSGSA-N U50488 Chemical compound N1([C@@H]2CCCC[C@H]2N(C)C(=O)CC=2C=C(Cl)C(Cl)=CC=2)CCCC1 VQLPLYSROCPWFF-QZTJIDSGSA-N 0.000 claims description 2
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- ZSDAQBWGAOKTSI-UNMCSNQZSA-N n-methyl-2-(3-nitrophenyl)-n-[(1s,2s)-2-pyrrolidin-1-yl-2,3-dihydro-1h-inden-1-yl]acetamide Chemical compound N1([C@@H]2[C@H](C3=CC=CC=C3C2)N(C)C(=O)CC=2C=C(C=CC=2)[N+]([O-])=O)CCCC1 ZSDAQBWGAOKTSI-UNMCSNQZSA-N 0.000 claims description 2
- KXMAIWXPZGQNCR-QGZVFWFLSA-N n-propyl-10-[(2r)-1-pyrrolidin-1-ylpropan-2-yl]phenothiazine-2-carboxamide Chemical compound C([C@@H](C)N1C2=CC=CC=C2SC2=CC=C(C=C21)C(=O)NCCC)N1CCCC1 KXMAIWXPZGQNCR-QGZVFWFLSA-N 0.000 claims description 2
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- A61K31/485—Morphinan derivatives, e.g. morphine, codeine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/5375—1,4-Oxazines, e.g. morpholine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
- A61K38/04—Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
- A61K38/07—Tetrapeptides
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/04—Centrally acting analgesics, e.g. opioids
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K2300/00—Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
Landscapes
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Epidemiology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Organic Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Biomedical Technology (AREA)
- Pain & Pain Management (AREA)
- Immunology (AREA)
- Gastroenterology & Hepatology (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Emergency Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201710242435 | 2017-04-14 | ||
| CN201710242435.0 | 2017-04-14 | ||
| PCT/CN2018/082912 WO2018188641A1 (zh) | 2017-04-14 | 2018-04-13 | 一种mor激动剂与kor激动剂的药物组合物及其用途 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CA3058272A1 true CA3058272A1 (en) | 2018-10-18 |
Family
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CA3058272A Abandoned CA3058272A1 (en) | 2017-04-14 | 2018-04-13 | Pharmaceutical composition containing mor agonist and kor agonist, and uses thereof |
Country Status (11)
| Country | Link |
|---|---|
| US (1) | US20200054594A1 (de) |
| EP (1) | EP3610874A4 (de) |
| JP (1) | JP2020516591A (de) |
| KR (1) | KR20190133047A (de) |
| CN (1) | CN109982699A (de) |
| AU (1) | AU2018251118A1 (de) |
| BR (1) | BR112019020691A2 (de) |
| CA (1) | CA3058272A1 (de) |
| MX (1) | MX2019011904A (de) |
| TW (1) | TW201836606A (de) |
| WO (1) | WO2018188641A1 (de) |
Families Citing this family (11)
| Publication number | Priority date | Publication date | Assignee | Title |
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| US11471503B2 (en) * | 2017-12-06 | 2022-10-18 | Jiangsu Hengrui Medicine Co., Ltd. | Use of KOR agonist in combination with MOR agonist in preparing drug for treating pain |
| CN111836807A (zh) * | 2018-04-28 | 2020-10-27 | 四川科伦博泰生物医药股份有限公司 | 氧杂螺环类化合物及其制备方法和用途 |
| WO2020147848A1 (zh) * | 2019-01-17 | 2020-07-23 | 上海海雁医药科技有限公司 | 三环取代的氧杂螺环衍生物、其制法与医药上的用途 |
| CN111662284B (zh) * | 2019-03-06 | 2021-08-10 | 上海海雁医药科技有限公司 | 双杂环取代的氧杂螺环衍生物、其制法与医药上的用途 |
| US20210040150A1 (en) * | 2019-08-07 | 2021-02-11 | Humanwell Pharmaceutical US | Kappa opioid receptor peptide amide agonists |
| CN112789276A (zh) * | 2019-08-14 | 2021-05-11 | 上海海雁医药科技有限公司 | 镇痛化合物、其制法与医药上的用途 |
| KR20220128428A (ko) * | 2020-01-17 | 2022-09-20 | 상하이 하이옌 파마슈티컬 테크놀로지 컴퍼니, 리미티드 | 아자비시클릭 치환된 옥사스피로 유도체, 이의 제조 방법 및 의학적 용도 |
| US20230147833A1 (en) * | 2020-01-17 | 2023-05-11 | Shanghai Haiyan Pharmaceutical Technology Co., Ltd. | Optically pure oxaspiro-substituted pyrrolopyrazole derivative, preparation method therefor and pharmaceutical use thereof |
| CN113214264B (zh) * | 2020-01-21 | 2022-08-09 | 上海海雁医药科技有限公司 | 二氢吡咯并五元杂芳基取代的氧杂螺环衍生物、其制法与医药上的用途 |
| CA3180729A1 (en) | 2020-06-25 | 2021-12-30 | Subo Liao | Peptides for treatment of medical disorders |
| EP4302779A1 (de) * | 2021-03-04 | 2024-01-10 | Socium Inc. | Krebstherapeutikum |
Family Cites Families (13)
| Publication number | Priority date | Publication date | Assignee | Title |
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| KR100648133B1 (ko) | 2005-04-25 | 2006-11-23 | 일동제약주식회사 | 펩티드 데포르밀라제 저해제로서 신규의 히드록사믹 산유도체 및 그 제조방법 |
| US8906859B2 (en) | 2006-11-10 | 2014-12-09 | Cera Therapeutics, Inc. | Uses of kappa opioid synthetic peptide amides |
| US7842662B2 (en) | 2006-11-10 | 2010-11-30 | Cara Therapeutics, Inc. | Synthetic peptide amide dimers |
| CN101627049B (zh) * | 2006-11-10 | 2012-09-05 | 卡拉治疗学股份有限公司 | 合成酞酰胺 |
| ME02754B (de) * | 2011-03-23 | 2018-01-20 | Trevena Inc | Opioidrezeptorliganden und verfahren zu ihrer verwendung und herstellung |
| EP2823409A4 (de) * | 2012-03-04 | 2015-12-02 | Adam Jeffries | Verarbeitung von datensystemen |
| WO2015065867A2 (en) | 2013-10-28 | 2015-05-07 | Cara Therapeutics, Inc. | Peripheral kappa opioid receptor agonists for preventing, inhibiting or treating nausea and vomiting |
| WO2016073443A2 (en) | 2014-11-05 | 2016-05-12 | Cara Therapeutics, Inc. | Peripheral kappa opioid receptor agonists for hard tissue pain |
| WO2016187537A1 (en) * | 2015-05-21 | 2016-11-24 | The Arizona Board Of Regents On Behalf Of The University Of Arizona | Multifunctional opioid receptor ligands and methods of treating pain |
| PT3354649T (pt) * | 2015-10-15 | 2020-02-03 | Jiangsu Hengrui Medicine Co | Derivado oxa espiro, seu método de preparação e suas aplicações em medicamentos |
| CN107098871B (zh) | 2016-02-23 | 2021-07-02 | 江苏恒瑞医药股份有限公司 | 苯基丙酰胺类衍生物、其制备方法及其在医药上的应用 |
| RS61193B1 (sr) * | 2017-04-14 | 2021-01-29 | Jiangsu hengrui medicine co ltd | So agonista opijatnog receptora (mor), kristalni oblik i fumaratne soli iste i postupak za njihovo dobijanje |
| US11471503B2 (en) * | 2017-12-06 | 2022-10-18 | Jiangsu Hengrui Medicine Co., Ltd. | Use of KOR agonist in combination with MOR agonist in preparing drug for treating pain |
-
2018
- 2018-04-13 KR KR1020197032604A patent/KR20190133047A/ko not_active Application Discontinuation
- 2018-04-13 EP EP18783681.2A patent/EP3610874A4/de not_active Withdrawn
- 2018-04-13 CA CA3058272A patent/CA3058272A1/en not_active Abandoned
- 2018-04-13 AU AU2018251118A patent/AU2018251118A1/en not_active Abandoned
- 2018-04-13 JP JP2019553307A patent/JP2020516591A/ja not_active Ceased
- 2018-04-13 MX MX2019011904A patent/MX2019011904A/es unknown
- 2018-04-13 CN CN201880004339.5A patent/CN109982699A/zh active Pending
- 2018-04-13 TW TW107112741A patent/TW201836606A/zh unknown
- 2018-04-13 WO PCT/CN2018/082912 patent/WO2018188641A1/zh active Application Filing
- 2018-04-13 BR BR112019020691-4A patent/BR112019020691A2/pt not_active Application Discontinuation
- 2018-04-13 US US16/499,931 patent/US20200054594A1/en not_active Abandoned
Also Published As
| Publication number | Publication date |
|---|---|
| EP3610874A1 (de) | 2020-02-19 |
| TW201836606A (zh) | 2018-10-16 |
| EP3610874A4 (de) | 2021-01-06 |
| MX2019011904A (es) | 2019-11-25 |
| WO2018188641A1 (zh) | 2018-10-18 |
| BR112019020691A2 (pt) | 2020-05-12 |
| CN109982699A (zh) | 2019-07-05 |
| JP2020516591A (ja) | 2020-06-11 |
| US20200054594A1 (en) | 2020-02-20 |
| KR20190133047A (ko) | 2019-11-29 |
| AU2018251118A8 (en) | 2019-10-31 |
| AU2018251118A1 (en) | 2019-10-17 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FZDE | Discontinued |
Effective date: 20231013 |